Weak links: Advancing target-based drug discovery by identifying the most vulnerable targets

Ann N Y Acad Sci. 2024 May;1535(1):10-19. doi: 10.1111/nyas.15139. Epub 2024 Apr 10.

Abstract

Mycobacterium tuberculosis remains the most common infectious killer worldwide despite decades of antitubercular drug development. Effectively controlling the tuberculosis (TB) pandemic will require innovation in drug discovery. In this review, we provide a brief overview of the two main approaches to discovering new TB drugs-phenotypic screens and target-based drug discovery-and outline some of the limitations of each method. We then explore recent advances in genetic tools that aim to overcome some of these limitations. In particular, we highlight a novel metric to prioritize essential targets, termed vulnerability. Stratifying targets based on their vulnerability presents new opportunities for future target-based drug discovery campaigns.

Keywords: CRISPRi; Mycobacterium tuberculosis; antibiotics; target‐based drug discovery; vulnerability.

Publication types

  • Review

MeSH terms

  • Antitubercular Agents* / pharmacology
  • Antitubercular Agents* / therapeutic use
  • Drug Discovery* / methods
  • Drug Discovery* / trends
  • Humans
  • Molecular Targeted Therapy / methods
  • Molecular Targeted Therapy / trends
  • Mycobacterium tuberculosis* / drug effects
  • Tuberculosis* / drug therapy

Substances

  • Antitubercular Agents